In vitro evaluation of apoptotic effect of bis(acetylacetonato-k2 O,O')(1,10-phenanthroline-k2 N,N')Zn(II) complex

Chem Biol Drug Des. 2017 Apr;89(4):529-537. doi: 10.1111/cbdd.12875. Epub 2016 Nov 2.

Abstract

Phenanthroline derivatives have been reported as potential bioactive compounds because of their ability to interact with DNA. To evaluate the antiproliferative effect of bis(acetylacetonate-k2 O,O)(1,10-phenanthroline-k2 N,N)Zn(II) or Zn(acac)2 (phen) complex, the compound was obtained in a simple manner and further characterized to determine crystal structure, thermal behavior, morphology, and spectroscopic properties. The structure of the complex was confirmed by X-ray single structure as well as by 1H and 13C nuclear magnetic resonance (NMR) in dmso-d6 (dimethyl sulfoxide) solution and in the solid state by 13C CP/MAS. Although preparation of this compound has been described previously, there are no reports on its biological activity; here, we assessed its antiproliferative effect on fibroblasts, A253, FaDu, Cal-27, RH-30, RD, U-373, C6, A-549, MDA-MB-231, and MCF-7 cancer cell lines at different doses (50-100 and 150 μg/ml). The cell viability was determined by MTT assay and high activity was observed for the most of the cell lines, and TUNEL results showed the induction of apoptosis.

Keywords: 1,10 phenanthroline; X-ray crystallography; carcinoma; infrared spectroscopy; zinc(II) acetylacetonate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Crystallography, X-Ray
  • Humans
  • In Situ Nick-End Labeling
  • In Vitro Techniques
  • Molecular Structure
  • Phenanthrolines / chemistry*
  • Phenanthrolines / pharmacology
  • Powder Diffraction
  • Spectrophotometry, Infrared
  • Zinc / chemistry*

Substances

  • Phenanthrolines
  • Zinc
  • 1,10-phenanthroline